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Salt, crystal form and preparation method of neurokinin-1 antagonist

A technology of crystal form and sodium salt, used in anti-inflammatory agents, nervous system diseases, organic chemical methods, etc., can solve problems such as difficult filtration, poor fluidity, and fine crystallization.

Pending Publication Date: 2022-06-28
SHANGHAI SHENGDI PHARMA CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Generally speaking, amorphous pharmaceutical products have no regular crystal structure and often have other defects, such as poor product stability, fine crystallization, difficult filtration, easy agglomeration, poor fluidity, etc.

Method used

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  • Salt, crystal form and preparation method of neurokinin-1 antagonist
  • Salt, crystal form and preparation method of neurokinin-1 antagonist
  • Salt, crystal form and preparation method of neurokinin-1 antagonist

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Example 1: Preparation of compound of formula II

[0069]

[0070] first step:

[0071]

[0072] in N 2 Under protection, compound 1 (2.43g, 4.86mmol, 1eq) was weighed in a 100mL three-necked flask, dissolved in dichloromethane (36mL), added diisopropylethylamine (5g, 38.76mmol, 8eq), cooled to - At 30° C., trimethylchlorosilane (1.36 g, 12.52 mmol, 2.6 eq) was added, and the mixture was stirred at room temperature for 2 h. Cool to -25°C, add dropwise a solution of chloromethyl chloroformate (0.77g, 6mmol, 1.23eq) in dichloromethane, control the temperature at -20°C to -5°C and stir until the reaction is complete, pour the reaction solution into ice water , separation, extraction with dichloromethane, adding water and 1N hydrochloric acid solution, separation, washing with brine, saturated aqueous sodium bicarbonate solution and brine successively, drying over anhydrous sodium sulfate, filtration, and concentration to obtain 3.0 g of yellow gum , the yield was ...

Embodiment 3

[0121] Embodiment 3 Stability investigation

[0122] The crystal form A of the sodium salt was placed at 4°C to investigate its stability, and the purity after being placed for 14 days was 99.18% (initial purity 99.25%). The results show that the sodium salt form A has good stability at 4℃.

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Abstract

The invention relates to a salt, a crystal form and a preparation method of a neurokinin-1 antagonist. Specifically, the invention relates to a sodium salt of a compound shown as a formula II, a crystal A of the sodium salt and a preparation method. The novel crystal form disclosed by the invention has good physicochemical properties and is more beneficial to clinical treatment.

Description

technical field [0001] The present disclosure relates to a salt, a crystal form of a neurokinin-1 antagonist and a preparation method thereof, in particular to the crystal form and preparation method of the sodium salt and sodium salt of the compound of formula II. Background technique [0002] Tachykinins are peptide ligands for neurokinin receptors. Neurokinin receptors, such as NK1, NK2 and NK3, are involved in various biological processes. They can be found in the nervous and circulatory systems of mammals as well as in surrounding tissues. Accordingly, modulation of such receptors has been investigated for potential treatment or prevention of various physiological disorders, conditions and diseases in mammals. [0003] On the other hand, drug hemolysis is caused by the massive destruction of red blood cells caused by immune factors after the drug enters the human body. Clinically, hemolytic phenomena such as anemia, jaundice, soy sauce and urine appear. Drug-induced ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6561A61P11/00A61P11/14A61P29/00A61P27/02A61P25/22A61P25/24A61P25/08A61P25/18A61P25/28A61P1/00A61P9/10A61P3/04A61P3/10A61P25/00A61P25/04A61P13/00A61P1/08A61P13/10A61P17/00A61P25/32A61K31/675
CPCC07F9/6561A61P11/00A61P11/14A61P29/00A61P27/02A61P25/22A61P25/24A61P25/08A61P25/18A61P25/28A61P1/00A61P9/10A61P3/04A61P3/10A61P25/00A61P25/04A61P13/00A61P1/08A61P13/10A61P17/00A61P25/32C07B2200/07C07B2200/13
Inventor 吴琪杨俊然杜振兴王捷
Owner SHANGHAI SHENGDI PHARMA CO LTD
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